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EP 0 594 795 A1

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(43) Date of publication: 04.05.1994 Bulletin 1994/18 (21) Application number: 92922789.0 (22) Date of filing: 10.04.1992

(51) International Patent Classification (IPC):  A61K 31/ 47( . ) A61K 36/ 00( . ) C07D 217/ 02( . ) C07D 217/ 06( . ) A61K 31/ 472( . ) A61P 31/ 12( . ) C07D 217/ 04( . ) C07D 217/ 08( . ) (86) International application number: PCT/US1992/002805 (87) International publication number: WO 1992/018125 (29.10.1992 Gazette 1992/27)

(84) Designated Contracting States: AT BE CH DE DK ES FR GB GR IT LI LU MC NL SE (30) Priority: 12.04.1991 US 19910684197 (71) Applicant: THE UNITED STATES OF AMERICA as represented by the Secretary United States Department of Commerce Springfield, Virginia 22161 (US)

(72) Inventors: BOYD, Michael R. Ijamsville, MD 21754 (US) CARDELLINA, John H., II Walkersville, MD 21793 (US) MANFREDI, Kirk P. Frederick, MD 21701 (US) BLUNT, John W. Christchurch 5 (NZ) PANNELL, Lewis K. Silver Spring, MD 20902 (US) MCMAHON, James B. Frederick, MD 21701 (US) GULAKOWSKI, Robert J. Germantown, MD 20874 (US) CRAGG, Gordon M. Bethesda, MD 20814 (US) (74) Representative: Smulders, Theodorus A.H.J., Ir., et al  Vereenigde Octrooibureaux Nieuwe Parklaan 97 NL-2587 BN 's-Gravenhage NL-2587 BN 's-Gravenhage (NL)